The steroid hormone 17β-estradiol (E2) is an important regulator of cell growth, differentiation, and physiological function of a diverse range of tissues. E2 exerts its biological effects on the target tissues through association with intracellular receptor proteins called estrogen receptors (ERs). Binding of E2 activates the receptor allowing it to interact with specific DNA sequences within the promoters of responsive genes and changes the gene expression profiles in target tissues. Identification of the ER laid the foundation for the discovery of an evolutionarily conserved family of receptors known as nuclear hormone receptors. Over the past 30years, research on ER biology has contributed a tremendous amount of unexpected and unimaginable wealth of information to the field of gene regulation and cell signaling as a whole. It is now well appreciated that the mechanism of ER action is multifaceted, involving multiple levels of complex regulation affecting gene transcription. This chapter summarizes our overall understanding of the molecular mechanism of ER action, beginning with the classical findings to the recent developments that have exposed several exciting themes that continue to enhance our understanding of ER signaling.
- Post-translational modification
- Ubiquitin-proteasome pathway
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